MedKoo Cat#: 585030 | Name: Pafenolol

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pafenolol is a beta 1-adrenoceptor antagonist studied in asthmatic patients.

Chemical Structure

Pafenolol
Pafenolol
CAS#75949-61-0

Theoretical Analysis

MedKoo Cat#: 585030

Name: Pafenolol

CAS#: 75949-61-0

Chemical Formula: C18H31N3O3

Exact Mass: 337.2365

Molecular Weight: 337.46

Elemental Analysis: C, 64.07; H, 9.26; N, 12.45; O, 14.22

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
Pafenolol
IUPAC/Chemical Name
(+-)-1-(p-(2-Hydroxy-3-(isopropylamino)propoxy)phenethyl)-3-isopropylurea
InChi Key
PKWZWSXSCKVUJB-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H31N3O3/c1-13(2)20-11-16(22)12-24-17-7-5-15(6-8-17)9-10-19-18(23)21-14(3)4/h5-8,13-14,16,20,22H,9-12H2,1-4H3,(H2,19,21,23)
SMILES Code
O=C(NC(C)C)NCCC1=CC=C(OCC(O)CNC(C)C)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 337.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Lennernäs H, Regårdh CG. Dose-dependent intestinal absorption and significant intestinal excretion (exsorption) of the beta-blocker pafenolol in the rat. Pharm Res. 1993 May;10(5):727-31. PubMed PMID: 8100631. 2: Löfdahl CG, Marlin GE, Svedmyr N. Pafenolol, a highly selective beta 1-adrenoceptor-antagonist, in asthmatic patients: interaction with terbutaline. Clin Pharmacol Ther. 1983 Jan;33(1):1-9. PubMed PMID: 6129091. 3: Dahlöf B, Sjöberg KH, Flygt C, Jern S, Hansen S, Hansson L. Pafenolol in hypertension: a double-blind randomized trial of a new beta 1-selective adrenoceptor blocker. J Cardiovasc Pharmacol. 1986 Jan-Feb;8(1):55-9. PubMed PMID: 2419693. 4: Lennernäs H, Renberg L, Hoffmann KJ, Regårdh CG. Presystemic elimination of the beta-blocker pafenolol in the rat after oral and intraperitoneal administration and identification of a main metabolite in both rats and humans. Drug Metab Dispos. 1993 May-Jun;21(3):435-40. PubMed PMID: 8100498. 5: Lennernäs H, Regårdh CG. Regional gastrointestinal absorption of the beta-blocker pafenolol in the rat and intestinal transit rate determined by movement of 14C-polyethylene glycol (PEG) 4000. Pharm Res. 1993 Jan;10(1):130-5. PubMed PMID: 8094244. 6: Lenneräs H, Regårdh CG. Pharmacokinetics of pafenolol in the rat: a suitable model for studying absorption mechanisms of a drug exhibiting unusual absorption properties in man. Biopharm Drug Dispos. 1990 Oct;11(7):619-31. PubMed PMID: 1979924. 7: Lennernäs H, Regårdh CG. Evidence for an interaction between the beta-blocker pafenolol and bile salts in the intestinal lumen of the rat leading to dose-dependent oral absorption and double peaks in the plasma concentration-time profile. Pharm Res. 1993 Jun;10(6):879-83. PubMed PMID: 8100633. 8: Regårdh CG, Lundborg P, Gabrielsson M, Heggelund A, Kylberg-Hanssen K. Pharmacokinetics of a single intravenous and oral dose of pafenolol--a beta 1-adrenoceptor antagonist with atypical absorption and disposition properties--in man. Pharm Res. 1990 Dec;7(12):1222-7. PubMed PMID: 1982773. 9: Sigurdsson JA, Bengtsson C, Bjurö T. Pafenolol, a new beta 1-selective blocking agent, in mild hypertension. Result of an inpatient study and a subsequent outpatient follow-up. Eur J Clin Pharmacol. 1984;26(5):549-53. PubMed PMID: 6147255. 10: Regardh CG, Heggelund A, Kylberg-Hanssen K, Lundborg P. Pharmacokinetics of pafenolol after i.v. and oral administration of three separate doses of different strength to man. Biopharm Drug Dispos. 1990 Oct;11(7):607-17. PubMed PMID: 1979923. 11: Berglund G, De Faire U, Castenfors J, Andersson G, Hartford M, Liedholm H, Ljungman S, Thulin T, Wikstrand J. Monitoring 24-hour blood pressure in a drug trial. Evaluation of a noninvasive device. Hypertension. 1985 Sep-Oct;7(5):688-94. PubMed PMID: 4040887. 12: Nyborg NC, Mikkelsen EO. Characterization of beta-adrenoceptor subtype in isolated ring preparations of intramural rat coronary small arteries. J Cardiovasc Pharmacol. 1985 Nov-Dec;7(6):1113-7. PubMed PMID: 2418297. 13: Ellingsen O, Sejersted OM, Leraand S, Ilebekk A. Catecholamine-induced myocardial potassium uptake mediated by beta 1-adrenoceptors and adenylate cyclase activation in the pig. Circ Res. 1987 Apr;60(4):540-50. PubMed PMID: 3036391. 14: Löfdahl CG, Marlin GE, Svedmyr N. The effects of pafenolol and metoprolol on ventilatory function and haemodynamics during exercise by asthmatic patients. Eur J Clin Pharmacol. 1983;24(3):289-95. PubMed PMID: 6134621. 15: Wong GW, Boyda HN, Wright JM. Blood pressure lowering efficacy of beta-1 selective beta blockers for primary hypertension. Cochrane Database Syst Rev. 2016 Mar 10;3:CD007451. doi: 10.1002/14651858.CD007451.pub2. Review. PubMed PMID: 26961574; PubMed Central PMCID: PMC6486283. 16: Rivera L, Hernández M, Benedito S, Prieto D, García-Sacristán A. Mediation of contraction and relaxation by alpha- and beta-adrenoceptors in the ureterovesical junction of the sheep. Res Vet Sci. 1992 Jan;52(1):57-61. PubMed PMID: 1348146. 17: Chiou WL, Ma C, Chung SM, Wu TC, Jeong HY. Similarity in the linear and non-linear oral absorption of drugs between human and rat. Int J Clin Pharmacol Ther. 2000 Nov;38(11):532-9. Erratum in: Int J Clin Pharmacol Ther 2001 Mar;39(3):138. PubMed PMID: 11097145. 18: Karlsson J, Kuo SM, Ziemniak J, Artursson P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br J Pharmacol. 1993 Nov;110(3):1009-16. PubMed PMID: 7905337; PubMed Central PMCID: PMC2175785. 19: Abrahamsson T. Characterization of the beta 1-adrenoceptor stimulatory effects of the partial beta 1-agonists acebutolol, xamoterol, H142/08 and H201/70. Eur J Pharmacol. 1989 May 2;164(1):121-8. PubMed PMID: 2568935. 20: Abrahamsson T. The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat. Br J Pharmacol. 1986 Apr;87(4):657-64. PubMed PMID: 2871880; PubMed Central PMCID: PMC1916803.